[Stocktaking of local anesthetics 2020].

Area of Science:

• Anesthesiology
• Pharmacology
• Regional Anesthesia

Background:

• Local anesthetics are foundational for regional anesthesia, acting primarily as sodium channel blockers.
• Their effects extend beyond sodium channels, influencing other targets and producing systemic effects.
• Adjuvants and novel formulations are explored to prolong anesthetic action and improve postoperative pain relief.

Purpose of the Study:

• To review the multifaceted roles of local anesthetics beyond sodium channel blockade.
• To discuss advancements in prolonging local anesthetic action, including ultralong-acting agents and adjuvants.
• To highlight strategies for managing local anesthetic-induced systemic toxicity.

Main Methods:

• Literature review of local anesthetic mechanisms, pharmacology, and clinical applications.
• Discussion of adjuvants (opioids, corticosteroids, α2-agonists) and ultralong-acting formulations (liposomal bupivacaine).
• Overview of local anesthetic-induced systemic toxicity and its management, including lipid emulsion therapy.

Main Results:

• Local anesthetics interact with multiple ion channels and cellular structures, contributing to efficacy and systemic effects.
• Adjuvants and liposomal bupivacaine show potential for extended nerve blockade, possibly rivaling continuous techniques.
• Systemic toxicity, though rare, necessitates careful administration and prompt treatment with lipid emulsions.

Conclusions:

• Local anesthetics possess complex pharmacology beyond sodium channel blockade, offering therapeutic advantages.
• Innovations in local anesthetic delivery and adjuvants aim to optimize postoperative analgesia.
• Safe clinical practice requires vigilance regarding systemic toxicity and preparedness for its management.